乌头原碱
| 中文名称 | 乌头原碱 |
|---|---|
| 中文同义词 | 烏頭原鹼;乌头原碱;乌头原碱(标准品);乌头原碱(滴定法95%);ACONINE 乌头原碱;乌头原总碱;WTYJ对照品;乌头原碱(对照品) |
| 英文名称 | ACONINE |
| 英文同义词 | ACONINE;(15S,16S)-20-Ethyl-1α,6α,16-trimethoxy-4-(methoxymethyl)aconitane-3α,8β,13β,14α,15-pentol;20-Ethyl-1α,6α,16β-trimethoxy-4-(methoxymethyl)aconitane-3α,8,13,14α,15α-pentol;(1alpha,3alpha,6alpha,14alpha,15alpha,16beta)-20-Ethyl-1,6,16-trimethoxy-4-(methoxymethyl)aconitane-3,8,13,14,15-pentol;Jesaconine;Aconitane-3,8,13,14,15-pentol,20-ethyl-1,6,16-trimethoxy-4-(methoxymethyl)-, (1a,3a,6a,14a,15a,16b)-;Aconine (Jesaconine);Aconitane-3,8,13,14,15-pentol, 20-ethyl-1,6,16-trimethoxy-4-(methoxymethyl)-, (1α,3α,6α,14α,15α,16β)- |
| CAS号 | 509-20-6 |
| 分子式 | C25H41NO9 |
| 分子量 | 499.6 |
| EINECS号 | |
| 相关类别 | 生物碱;中草药成分;植物提取物;中药对照品;标准品;chemical reagent;pharmaceutical intermediate;phytochemical;reference standards from Chinese medicinal herbs (TCM).;对照品;植提标准品;Alkaloids;标准品-中药标准品;标准品 -中药标准品;标准品，对照品;standardized herbal extract |
| Mol文件 | 509-20-6.mol |
| 结构式 |  |
乌头原碱 性质
| 熔点 | 129-131℃ |
|---|---|
| 比旋光度 | D +23° |
| 沸点 | 590.79°C (rough estimate) |
| 密度 | 1.42 |
| 折射率 | 1.6000 (estimate) |
| 储存条件 | -20°C Freezer |
| 溶解度 | 可溶于氯仿（少许）、DMSO（少许） |
| 酸度系数(pKa) | 9.52(at 25℃) |
| 形态 | 固体 |
| 颜色 | 灰白色至浅黄色 |
1）提取：草乌中主要成分为乌头碱生物碱，将干燥草乌块根约4.8kg粉碎至约过1～2号筛，粉碎的颗粒分装到6L的分液漏斗中，用1000mL25％的氨水浸泡药材2～4小时，再用二氯甲烷浸泡草乌颗粒药材，浸泡24小时，每隔两天渗漉一次，总共提取4次，减压回收溶剂，合并浸膏，称重得膏率为20.10～23.20g/kg，浸膏4℃保存备用。用18-19％的HCl溶液超声溶解草乌浸膏，过滤水液层除去草乌中油状物，用约40％NaOH溶液沉淀水液层，大量黄白色沉淀出现，放冷，过滤沉淀，沉淀冷冻干燥，称重得黄白色沉淀为7.2～7.9g/kg，4℃保存备用。
2）乌头原碱的分离：取部分NaOH碱液的黄白色沉淀用200-300目硅胶分离，用正己烷/乙酸乙酯为流动相，冲洗硅胶色谱柱。用薄层色谱跟踪乌头碱至乌头碱的点消失即停止柱分离。所得的乌头碱粗品经二氯甲烷重结晶得到乌头原碱纯品。
Aconine 抑制核因子 κB 受体活化剂配体诱导的 NF-κB 激活。|
NF-κB
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Treatment with Aconine significantly inhibits the RANKL-induced transcriptional activity of NF-κB in a dose-dependent manner. Aconine inhibits RANKL-induced osteoclast differentiation in RAW264.7 cells by suppressing the activation of NF-κB and NFATc1 and the expression of the cell-cell fusion molecule DC-STAMP. Aconine (0.125, 0.25 μM) does not affect the viability of RAW264.7 cells, but dose-dependently inhibits RANKL-induced osteoclast formation and bone resorptive activity. Aconine dose-dependently inhibits the RANKL-induced activation of NF-κB and NFATc1 in RAW264.7 cells, and subsequently reduces the expression of osteoclast-specific genes (c-Src, β3-Integrin, cathepsin K and MMP-9) and the expression of dendritic cell-specific transmembrane protein (DC-STAMP), which plays an important role in cell-cell fusion.